Tìm theo
Demecarium
Các tên gọi khác (1) :
  • Demecarium
cholinergic agents
Thuốc Gốc
Small Molecule
ATC: S01EB04
ĐG : Dispensing Solutions , http://www.drxdispensing.com
CTHH: C32H52N4O4
PTK: 556.7797
Demecarium is an indirect-acting parasympathomimetic agent that is used to treat glaucoma. It is a cholinesterase inhibitor or an anticholinesterase. Cholinesterase inhibitors prolong the effect of acetylcholine, which is released at the neuroeffector junction of parasympathetic postganglion nerves, by inactivating the cholinesterases that break it down. Demecarium inactivates both pseudocholinesterase and acetylcholinesterase. In the eye, this causes constriction of the iris sphincter muscle (causing miosis) and the ciliary muscle. The outflow of the aqueous humor is facilitated, which leads to a reduction in intraocular pressure.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C32H52N4O4
Phân tử khối
556.7797
Monoisotopic mass
556.398856172
InChI
InChI=1S/C32H52N4O4/c1-33(31(37)39-29-21-17-19-27(25-29)35(3,4)5)23-15-13-11-9-10-12-14-16-24-34(2)32(38)40-30-22-18-20-28(26-30)36(6,7)8/h17-22,25-26H,9-16,23-24H2,1-8H3/q+2
InChI Key
InChIKey=RWZVPVOZTJJMNU-UHFFFAOYSA-N
IUPAC Name
N,N,N-trimethyl-3-{[methyl(10-{methyl[3-(trimethylazaniumyl)phenoxycarbonyl]amino}decyl)carbamoyl]oxy}anilinium
Traditional IUPAC Name
demarcarium
SMILES
CN(CCCCCCCCCCN(C)C(=O)OC1=CC=CC(=C1)[N+](C)(C)C)C(=O)OC1=CC=CC(=C1)[N+](C)(C)C
Độ tan chảy
164-170
Độ hòa tan
1.69e-05 g/l
logP
-1.75
logS
-7.6
PSA
59.08 Å2
Refractivity
185.71 m3·mol-1
Polarizability
64.49 Å3
Rotatable Bond Count
17
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
2
Number of Rings
2
Bioavailability
0
Dược Lực Học : Demecarium is a long-acting cholinesterase inhibitor and potent miotic. Because of its toxicity, it should be reserved for use in patients with open-angle glaucoma or other chronic glaucomas not satisfactorily controlled with the short-acting miotics and other agents. Application of demecarium to the eye produces intense miosis and ciliary muscle contraction due to inhibition of cholinesterase, allowing acetylcholine to accumulate at sites of cholinergic transmission. These effects are accompanied by increased capillary permeability of the ciliary body and iris, increased permeability of the blood-aqueous barrier, and vasodilation. Myopia may be induced or, if present, may be augmented by the increased refractive power of the lens that results from the accommodative effect of the drug.
Cơ Chế Tác Dụng : Demecarium is an indirect-acting parasympathomimetic agent that is used to treat glaucoma. It is a cholinesterase inhibitor or an anticholinesterase. Cholinesterase inhibitors prolong the effect of acetylcholine, which is released at the neuroeffector junction of parasympathetic postganglion nerves, by inactivating the cholinesterases that break it down. Demecarium inactivates both pseudocholinesterase and acetylcholinesterase. In the eye, this causes constriction of the iris sphincter muscle (causing miosis) and the ciliary muscle. The outflow of the aqueous humor is facilitated, which leads to a reduction in intraocular pressure. Demecarium is an indirect-acting parasympathomimetic agent, also known as a cholinesterase inhibitor and anticholinesterase. Cholinesterase inhibitors prolong the effect of acetylcholine, which is released at the neuroeffector junction of parasympathetic postganglion nerves, by inactivating the cholinesterases that break it down. Demecarium inactivates both pseudocholinesterase and acetylcholinesterase. In the eye, this causes constriction of the iris sphincter muscle (causing miosis) and the ciliary muscle (affecting the accommodation reflex and causing a spasm of the focus to near vision). The outflow of the aqueous humor is facilitated, which leads to a reduction in intraocular pressure. Of the two actions, the effect on the accommodation reflex is the more transient and generally disappears before termination of the miosis.
Độc Tính : The oral LD50 is 2.96 mg/kg in the mouse. Symptoms of overdose include nausea, vomiting, abdominal cramps, diarrhea, urinary incontinence, salivation, sweating, difficulty in breathing, bradycardia, or cardiac irregularities.
Chỉ Định : For the topical treatment of chronic open-angle glaucoma.
Tương Tác Thuốc :
  • Tacrine The acetylcholinesterase inhibitor, Tacrine, may increase the adverse/toxic effects of Demcarium, a cholinergic agonist. Monitor for increased cholinergic effects and toxicity.
Liều Lượng & Cách Dùng : Solution - Ophthalmic
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : MSD
    Sản phẩm biệt dược : Humorsol
  • Công ty :
    Sản phẩm biệt dược : Tonilen
  • Công ty :
    Sản phẩm biệt dược : Tosmilen
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00944
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5965
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507824
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00667
PharmGKB
http://www.pharmgkb.org/drug/PA164745610
Wikipedia
http://en.wikipedia.org/wiki/Demecarium_bromide
RxList
http://www.rxlist.com/cgi/generic2/demecarium.htm
Drugs.com
http://www.drugs.com/mtm/demecarium-bromide-ophthalmic.html
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